SRT 1460

SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5 > 300 μM), and is more potent than Resveratrol and the closest sirtuin homologues[1].

Signaling Pathways >> Epigenetics >> Sirtuin

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Sirtuin

SIRT1:2.9 μM (EC1.5)

SRT 1460 (2-6 μM; 72 hours) inhibits cell viability in a dose-dependent manner, with all pancreatic cancer cells being more sensitive than the control HPDE cell. The IC50s of those cells are: Patu8988t, 1.62±0.13 μM; SU86.86, 2.31±0.23 μM; Panc-1, 0.66 ±0.02 μM; HPDE, 2.39±0.29 μM[2]. SRT 1460 (5 μM; 16 hours) increases expression of the autophagy marker LC3-II[2]. Cell Viability Assay[2] Cell Line: Patu8988t (pancreatic cancer cells), Panc-1 (pancreatic cancer cells), SU86.86 (pancreatic cancer cells), HPDE cells Concentration: 2 μM, 4 μM, 6 μM Incubation Time: 72 hours Result: Inhibited cell viability in a dose-dependent manner, with all pancreatic cancer cells being more sensitive than the control HPDE cell. The IC50s of those cells were: Patu8988t, 1.62±0.13 μM; SU86.86, 2.31±0.23 μM; Panc-1, 0.66 ±0.02 μM; HPDE, 2.39±0.29 μM. Western Blot Analysis[2] Cell Line: Patu8988t cells Concentration: 5 μM Incubation Time: 16 hours Result: SRT1460 increased expression of the autophagy marker LC3-II.

[1]. Milne JC, et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29; 450(7170): 712–716.

[2]. Chini CC, et al. SIRT1-Activating Compounds (STAC) Negatively Regulate Pancreatic Cancer Cell Growth and Viability Through a SIRT1 Lysosomal-Dependent Pathway. Clin Cancer Res. 2016 May 15;22(10):2496-507.